Suprastinex - instructions for use, dose, side effects, contraindications

auxiliary substances: silicon microcrystalline cellulose (Prosolv® HD90) 40.4 mg (microcrystalline cellulose (98%), silicon dioxide colloidal anhydrous (2%)), lactose monohydrate 37.9 mg, low-substituted giprolose (L-HPC 11) 10 mg, magnesium stearate 1.7 mg; shell; Opapray II 33G28523 white 5 mg (hypromellose 2910 (40%), titanium dioxide (25%), lactose monohydrate (21 %) 1.05 mg, macrogol 3350 (8%), triacetin (6%)).

Description:White or nearly white round biconvex tablets coated with a film sheath, engraved "E" on one side of the tablet and "281" on the other side, without or almost odorless.

Pharmacotherapeutic group:Antiallergic agent - H1-histamine receptor blocker

ATX: & nbsp

R.06.A.E. Piperazine derivatives

E.06.A.E.09 Levocetirizine

Pharmacodynamics:

Antiallergic agent. Enantiomer of cetirizine; a competitive histamine antagonist; blocks H1-histamine receptors, affinity for which is 2 times higher than that of cetirizine. Has an effect on the histamine-dependent stage of allergic reactions; reduces the migration of eosinophils, reduces vascular permeability, limits the release of inflammatory mediators.

Prevents development and facilitates the course of allergic reactions, has antiexudative (decongestant), antipruritic effect; practically does not have anticholinergic and antiserotonergic action.In therapeutic doses, it practically does not have a sedative effect.

Pharmacokinetics:

Pharmacokinetics is linear. Quickly absorbed when taken orally; food intake does not affect the fullness of absorption, but reduces its speed. Bioavailability - 100 %. Time to reach the maximum concentration (TCmax) is about 0.9 h, the maximum concentration (Cmah) - 207 ng / ml. The volume of distribution is about 0.4 l / kg.

Connection with proteins - 90 %. Less than 14% of the drug is metabolized in the liver by O-dealkylation to form a pharmacologically inactive metabolite. The half-life (T1 / 2) is 7-10 hours. The total clearance is about 0.63 ml / min / kg. It is completely eliminated from the body in 96 hours. It is excreted by the kidneys (approximately 85%). With renal insufficiency (creatinine clearance less than 40 ml / min), clearance decreases (in patients on hemodialysis - by 80%), T1 / 2 - lengthens. Less than 10% is removed during hemodialysis. Penetrates into breast milk.

Indications:

Symptomatic treatment of year-round (persistent) and seasonal allergic rhinitis and conjunctivitis (itching, sneezing, rhinorrhea, lacrimation, congestion hyperemia); hay fever (hay fever); urticaria, incl. chronic idiopathic urticaria; edema of Quincke; allergic dermatoses, accompanied by itching and rashes.

Contraindications:

Hypersensitivity to the active (including to piperazine derivatives) or any auxiliary component of the drug; severe renal failure (creatinine clearance less than 10 ml / min); children under 6 years of age (for this dosage form); pregnancy and lactation; lactose intolerance, hereditary lactase deficiency or glucose-galactose malabsorption syndrome.

Carefully:

Chronic renal failure of mild to moderate severity, elderly age (glomerular filtration may be reduced).

Pregnancy and lactation:

The use of the drug in pregnancy is contraindicated, since controlled clinical studies on the safety of the drug in pregnant women have not been conducted. If it is necessary to use the drug in lactation, it is recommended to stop breastfeeding.

Dosing and Administration:

For oral administration. The drug should be taken with food or on an empty stomach, with a small amount of water, without chewing.

The daily dose is recommended at one time.

The recommended dose for adults and children over 6 years old, elderly patients (with normal kidney function) is 5 mg (1 tablet) per day. The maximum daily dose should not exceed 5 mg.

Patients with impaired renal function

The frequency of admission is set by the doctor individually in accordance with a violation of kidney function. In patients with chronic renal insufficiency with the clearance of creatinine (CC) from 30 to 49 ml / min dose should be reduced by 2 times (5 mg (1 tablet) every other day); with QC from 10 to 29 ml / min dose should be reduced by 3 times (5 mg (1 tablet) every 3 days). In severe renal failure (CC less than 10 ml / min), the drug is contraindicated.

Patients with impaired hepatic function

When prescribing the drug to patients with an isolated impairment of liver function, no dose changes are required. Patients with combined disorders of the liver and kidneys are recommended dose adjustment (see the section "Patients with impaired renal function" above).

Duration of the drug

Duration of admission depends on the disease.

In the treatment of persistent allergic rhinitis (symptoms <4 days / 1 week or less than 4 weeks), treatment is continued until symptoms disappear; If symptoms appear, treatment can be resumed.In the treatment of seasonal allergic rhinitis (symptoms> 4 days / 1 week or longer than 4 weeks) treatment continues throughout the exposure period of allergens.

The course of treatment is determined by a doctor; on average, it is 1-6 weeks.

In chronic diseases (including chronic idiopathic urticaria), the course of treatment can be longer in agreement with the doctor.

There is a clinical experience of using the drug for up to 6 months.

Side effects:

The parameters used below for the frequency of side effects are defined as follows: very often -> 1/10; often - <1/10 and> 1/100; infrequently - <1/100 and> 1/1000; rarely - <1/1000 and> 1/10000; very rarely - <1/10000.

From the immune system: very rarely - allergic reactions, including anaphylaxis.

From the side of metabolism: very rarely - weight gain.

From the central and peripheral nervous system: often - drowsiness, headache, increased fatigue; infrequently - asthenia; rarely - migraine, dizziness.

On the part of the respiratory system: very rarely - dyspnoea.

From the gastrointestinal tract: often - dry mouth; infrequently - abdominal pain; very rarely - nausea, indigestion.

From the subcutaneous fat: very rarely - angioedema, skin itching, rash, urticaria.

From the laboratory indicators: very rarely - a change in functional "liver" samples.

If any side effects occur, incl. not specified in the instructions, you need to see a doctor.

Overdose:

Symptoms of overdose in adults are drowsiness, in children - excitement, anxiety, which are replaced by drowsiness. In case of an overdose, it is necessary to rinse and stomach and consult a doctor. There is no specific antidote. Symptomatic and supportive therapy is recommended. Hemodialysis is ineffective.

Interaction:

Studies of the interactions of levocetirizine showed no clinically significant interactions with pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide, and diazepam. Joint use with macrolides or ketoconazole did not cause significant changes in the ECG.

Theophylline (400 mg / day) reduces the total clearance of levocetirizine by 16%, while the kinetics of theophylline does not change.

Levocetirizine does not enhance the effects of alcohol, but in sensitive patients, concomitant administration of levocetirizine with alcohol or other CNS depressant agents may affect the CNS.

Special instructions:

During treatment it is recommended to refrain from using ethanol.

The preparation of Suprastinex® coated tablets contains lactose, so it should not be administered to patients with lactose intolerance, hereditary lactase deficiency, or glucose-galactose malabsorption syndrome.

Effect on the ability to drive transp. cf. and fur:

During the treatment period it is recommended to refrain from engaging in potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:Film coated tablets 5 mg.

Packaging:

Film coated tablets 5 mg: 7 or 10 tablets in a blister of polyamide / aluminum foil / PVC // aluminum foil. 1 or 2 blisters (7 tablets each) or 1, 2 or 3 blisters (10 tablets each) are packed together with instructions for use in a cardboard box.

Storage conditions:At a temperature of no higher than 30 ° C. Keep out of the reach of children.

Shelf life:5 years.
Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LSR-008568/10

Date of registration:23.08.2010

The owner of the registration certificate:EGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Manufacturer: & nbsp

EGIS PHARMACEUTICALS, Plc Hungary

Representation: & nbspEGIS ZAO Pharmaceutical Plant EGIS ZAO Pharmaceutical Plant Hungary

Information update date: & nbsp29.10.2015

Illustrated instructions

Instructions

Suprastinex® (Suprastinex®)